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statins, ezetimibe
Statins inhibit HMG-CoA reductase to reduce cholesterol synthesis, while ezetimibe blocks intestinal cholesterol absorption, together lowering LDL cholesterol levels.
Statins inhibit HMG-CoA reductase to reduce cholesterol synthesis, while ezetimibe blocks intestinal cholesterol absorption, together lowering LDL cholesterol levels. Used for Hypercholesterolemia and dyslipidemia for cardiovascular risk reduction, Primary and secondary prevention of coronary artery disease.
At a glance
| Generic name | statins, ezetimibe |
|---|---|
| Sponsor | Korea University Anam Hospital |
| Drug class | HMG-CoA reductase inhibitor and cholesterol absorption inhibitor combination |
| Target | HMG-CoA reductase; NPC1L1 transporter |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
Mechanism of action
Statins competitively inhibit HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol synthesis, reducing intracellular cholesterol and upregulating LDL receptors for increased clearance. Ezetimibe selectively inhibits the Niemann-Pick C1-like 1 (NPC1L1) transporter in the intestinal brush border, preventing dietary and biliary cholesterol absorption. Combined, they provide complementary lipid-lowering effects through distinct mechanisms.
Approved indications
- Hypercholesterolemia and dyslipidemia for cardiovascular risk reduction
- Primary and secondary prevention of coronary artery disease
Common side effects
- Myalgia or muscle pain
- Elevated liver transaminases
- Headache
- Gastrointestinal upset
- Rhabdomyolysis
Key clinical trials
- A Study of Bempedoic Acid/Ezetimibe/High-intensity Statin in Patients Without Cardiovascular Events (PHASE3)
- Cholesterol Disruption in Combination With the Standard of Care in Patients With Advanced Pancreatic Adenocarcinoma (EARLY_PHASE1)
- Moderate-intensity Statin vs. Individualized LDL-C Target-based Therapy in Older Adults With Type 2 Diabetes (iTARGET-Elderly Study) (NA)
- Assessing the Impact of Intensification of Lipid Lowering Therapy With Guidelines-based Evinacumab Administration on Coronary Plaque Volumes Measured by Coronary Computed Tomography Angiography (CCTA) in Patients With Homozygous Familial Hypercholesterolemia (HoFH)
- Efficacy and Safety of Pitavastatin/Ezetimibe After Switching From Statin Monotherapy to Pitavastatin/Ezetimibe in Patients With Hypercholesterolemia
- triPle Oral thERapy With Bempedoic Acid vs uSual Care in Early Lipid Management of Patients With acUte coronAry synDromE (PHASE3)
- Optimal Antiplatelet and Lipid Therapy in ACS With DES: OPACT Trial (NA)
- Evolocumab in Patients With Multivessel Coronary Disease After Acute Myocardial Infarction: A Target Trial Emulation
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |